Synthesis of N-(3-arylprop-2-ynyl)substituted olanzapine derivatives as potential inhibitors of PDE4B

P. Vijaya Babu, Dhilli Rao Gorja, Chandana Lakshmi T Meda, Girdhar Singh Deora, Sunder Kumar Kolli, Kishore V L Parsa, K. Mukkanti, Manojit Pal

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Abstract

The linkage between dopamine D2 receptors and PDE activity via cAMP prompted us to design a series of novel N-(3-arylprop-2-ynyl)substituted olanzapine derivatives as potential inhibitors of PDE4B. The target compounds were conveniently prepared by using a simple and inexpensive method involving Pd/C-mediated CC bond forming reaction under Sonogashira conditions. A number of compounds were synthesized by using this strategy in good yields. Some of the compounds showed promising inhibition of PDE4B when tested in vitro that was supported by the docking studies. 

Original languageEnglish
Pages (from-to)3176-3180
Number of pages5
JournalTetrahedron Letters
Volume55
Issue number20
DOIs
Publication statusPublished - 14 May 2014
Externally publishedYes

Keywords

  • Alkyne
  • Docking
  • Olanzapine
  • PDE4

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